Chronic alcoholic liver disease: Use with caution; known to increase rosuvastatin exposure

Dosing Considerations

Initiating therapy or switching from another HMG-CoA reductase inhibitor: Start on appropriate dose and then titrate based on patient’s response and individualized goal of therapy

Limitation of use: Not studied in Fredrickson type I and V dyslipidemias

Dosage Forms & Strengths

tablet

5mg

10mg

20mg

40mg

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Familial Hypercholesterolemia

Heterozygous

Adjunctive therapy to diet to reduce total cholesterol, LDL cholesterol, and ApoB levels in children and adolescents (8-17 years) with heterozygous familial hypercholesterolemia after an inadequate response to diet therapy

Inadequate response defined as when the following findings are present: LDL cholesterol >190 mg/dL OR >160 mg/dL with a positive family history of premature cardiovascular disease (CVD) or ≥2 CVD risk factors

Adjunctive therapy to diet to reduce LDL cholesterol, total cholesterol, non-HDL cholesterol, and ApoB in children and adolescents (7-17 year) with homozygous familial hypercholesterolemia, either alone or with other lipid-lowering treatments (eg, LDL apheresis)

Increases in AST or ALT reported with HMG-CoA reductase inhibitors; monitor liver enzymes before initiating and if signs or symptoms of liver injury occur

Cases of myopathy and rhabdomyolysis with acute renal failure secondary to myoglobinuria reported with HMG-CoA reductase inhibitors; may occur at any dose level, but are increased at the highest dose (40 mg); caution in patients with predisposing factors for myopathy (eg, age ≥65 years, inadequately treated hypothyroidism, renal impairment)

Discontinue treatment if markedly elevated creatine kinase levels occur or myopathy is diagnosed or suspected; temporarily withhold in any patient with an acute, serious condition suggestive of myopathy or predisposing to the development of renal failure secondary to rhabdomyolysis (eg, sepsis; hypotension; dehydration; major surgery; trauma; severe metabolic, endocrine, or electrolyte disorders; uncontrolled seizures)

Pharmacokinetic studies demonstrated an ~2-fold elevation in median exposure (AUC and peak plasma concentrations) in Asian subjects when compared with a white control group

Rule out secondary causes of hyperlipidemia prior to initiating therapy

Drug interactions overview

Exercise caution when anticoagulants coadministered with rosuvastatin because of its potentiation of effect of coumarin-type anticoagulants in prolonging the prothrombin time/INR; monitor INR at baseline and frequently during concomitant therapy

Cyclosporine and gemfibrozil increased rosuvastatin exposure and may result in increased risk of myopathy

Coadministration of rosuvastatin with certain protease inhibitors has differing effects on rosuvastatin exposure and may increase risk of myopathy

Risk of skeletal muscle effects may be enhanced when used in combination with lipid-modifying doses (≥1 g/day) of niacin; use with caution when administered with rosuvastatin

Because the risk of myopathy during treatment with HMG-CoA reductase inhibitors is increased with concomitant use of fenofibrates, use with caution

Cases of myopathy, including rhabdomyolysis, reported with HMG-CoA reductase inhibitors when coadministered with colchicine

Lactation

Contraindicated

Limited data indicate that rosuvastatin is present in human milk; because statins have the potential for serious adverse reactions in nursing infants, women who require rosuvastatin treatment should not breastfeed their infants

Pregnancy Categories

A:Generally acceptable. Controlled studies in pregnant women show no evidence of fetal risk.

B:May be acceptable. Either animal studies show no risk but human studies not available or animal studies showed minor risks and human studies done and showed no risk.

C:Use with caution if benefits outweigh risks. Animal studies show risk and human studies not available or neither animal nor human studies done.

This polymorphism is proposed to reduced transport into the liver, the main site of statin metabolism and elimination, resulting in elevated plasma concentrations

SLCO1B1 polymorphism is thought to have a lesser effect on the more hydrophilic statins (eg, rosuvastatin, fluvastatin) compared with those that are more lipophilic (eg, atorvastatin, pravastatin, simvastatin)

Other genetic polymorphisms of elimination (eg, CYP450, P-glycoprotein) for each individual drug must also be considered, to explain variability for statin clearance among patients that exhibit SCLO1B1 polymorphism

SLCO1B1 CC genotype is most common in Caucasians and Asians
(15%); decrease dose by 50% in people of Asian descent

Risk of myopathy is 2.6- to 4.3-fold higher if the C allele is present and 16.9-fold higher in CC homozygotes than in TT homozygotes

Genetic testing laboratories

Optivia Biotechnology, Inc (http://optiviabio.com)

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Administration

Oral Administration

Take with or without food

Tablets: Swallow whole

Capsules

Swallow whole; do not crush or chew

For patients who have difficulty swallowing capsules

May open capsule and carefully empty granules onto 1 tsp of applesauce; swallow immediately, without chewing

Do not store mixture for future use

If not used in its entirety, discard remaining contents immediately

Nasogastric Tube Administration

Open capsule and empty granules into a 60-mL catheter-tipped syringe and add 40 mL of water

Shake syringe vigorously for 15 seconds; granules may start dissolving which is acceptable

Attach syringe to a nasogastric tube (≥16-French) and deliver contents of syringe through nasogastric tube

After administering granules, flush nasogastric tube with 20 mL of additional water

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The above information is provided for general
informational and educational purposes only. Individual plans may vary
and formulary information changes. Contact the applicable plan
provider for the most current information.

View explanations for tiers and
restrictions

Tier

Description

1

This drug is available at the lowest co-pay. Most
commonly, these are generic drugs.

2

This drug is available at a middle level co-pay. Most
commonly, these are "preferred" (on formulary) brand drugs.

3

This drug is available at a higher level co-pay. Most
commonly, these are "non-preferred" brand drugs.

4

This drug is available at a higher level co-pay. Most
commonly, these are "non-preferred" brand drugs or specialty
prescription products.

5

This drug is available at a higher level co-pay. Most
commonly, these are "non-preferred" brand drugs or specialty
prescription products.

6

This drug is available at a higher level co-pay. Most
commonly, these are "non-preferred" brand drugs or specialty
prescription products.

NC

NOT COVERED – Drugs that are not
covered by the plan.

Code

Definition

PA

Prior Authorization Drugs that
require prior authorization. This restriction requires that
specific clinical criteria be met prior to the approval of the
prescription.

QL

Quantity Limits Drugs that
have quantity limits associated with each prescription. This
restriction typically limits the quantity of the drug that will
be covered.

ST

Step Therapy Drugs that have
step therapy associated with each prescription. This restriction
typically requires that certain criteria be met prior to
approval for the prescription.

OR

Other Restrictions Drugs that
have restrictions other than prior authorization, quantity
limits, and step therapy associated with each prescription.